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Stereocomplexes of Triblock Poly(lactide- PEG2000-lactide) as Carrier of Drugs
Authors:Ashgan Bishara  Hans R Kricheldorf  Abraham J Domb
Institution:1. Department of Medicinal Chemistry and Nature Products, School of Pharmacy, Faculty of Medicine, Hebrew University of Jerusalem, Jerusalem, 91120 Israel;2. Institute of Technical and Macromolecular Chemistry, Hamburg University, Germany
Abstract:Triblock copolymers of poly(lactide)-poly(ethylene-glycol)-poly(lactide) (PLA-PEG2000-PLA) were synthesized by ring-opening polymerization of lactide and PEG2000 diol as co-catalyst. Stereocomplexes with particle sizes ranging from nanometers to microns were obtained by mixing acetonitrile solutions of pairs of enantiomeric homopoly(lactide) and the triblock copolymers. The stereocomplexes exhibited higher crystalline melting temperatures than the optically pure polymers. The ratio of PLA terminals in the copolymers had a significant effect on their stereocomplex degradation and drug release. These stereocomplexes were used for the encapsulation of dexamethasone for controlled release applications. Dexamethasone phosphate loading capacity, in vitro release, degradation and stability of polymers and formulation were investigated for one month. An increase in the dexamethsone phosphate content in the stereocomplex or a decrease in the PLA ratio in the copolymer resulted in a faster release of drug and polymer degradation.
Keywords:controlled release  degradation  dexamethasone phosphate  poly(ethylene glycol)  polylactide  stereocomplex
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